NOVEL DERIVATIVES OF 2,6-DIAMINOPYRIDIN-3-ONE Russian patent published in 2010 - IPC C07D213/73 A61K31/444 A61K31/4427 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention describes novel derivatives of 2,6-diaminopyridine of formula (I), where R¹ is piperidine which is optionally substituted with up to four substitutes independently selected from a group comprising: (a) hydrogen, (b) lower alkyl, (c) lower alkyl substituted with an oxo group or aryl, (d) CO₂R⁷, (e) COR¹², (f) C(O)NR¹³R¹⁴, and (g) S(O)_nR¹⁵; R² is phenyl which can be substituted with up to four substitutes independently selected from a group comprising: (a) lower alkyl, (b) lower alkyl substituted with a halide or OR¹⁰, (c) halide, or (d) OR¹²; R⁵ and R⁶ are independently selected from a group comprising (a) hydrogen and (b) lower alkyl; R⁷ is selected from a group comprising (a) hydrogen and (b) lower alkyl; R¹⁰ is selected from a group comprising (a) lower alkyl, (b) aryl and (c) aryl substituted with a halide or NR⁵R⁶; R¹² is selected from a group comprising (a) hydrogen and (b) lower alkyl; R¹³ and R¹⁴ are independently selected from a group comprising (a) hydrogen and (b) lower alkyl, R¹⁵ is selected from a group comprising (a) aryl, (b) aryl substituted with a halide, CO₂R¹², SO₂R¹⁰, COR¹², lower alkyl or lower alkyl substituted with a halide, OR¹², oxo group, CO₂R¹², C(O)NR⁵R⁶ or NR⁵R⁶, (c) heteroaryl, (d) heteroaryl substituted with a halide, CO₂R¹², SO₂R¹⁰, COR¹², lower alkyl and lower alkyl substituted with a halide, OR¹², oxo group, CO₂R¹², C(O)NR⁵R⁶ or NR⁵R⁶, (e) NR⁵R⁶, (f) lower alkyl, (g) lower alkyl substituted with a halogen, OR¹², oxo group, CO₂R¹², C(O)NR⁵R⁶ or NR⁵R⁶, (h) a heterocycle and (i) a heterocycle substituted with CO₂R¹², COR¹², SO₂R¹⁰, lower alkyl, C(O)NR⁵R⁶ or NR⁵R⁶; n equals 0, 1 or 2; as well as a pharmaceutical composition having inhibitory effect on cyclin-dependant kinase and a method of producing the compound of formula I.

EFFECT: novel compounds which have antiproliferative activity and can be used for treating or curbing cancer are obtained and described.

28 cl, 58 ex, 4 tbl